RESUMO
Phytochemical investigation on the whole plant of Chloranthus japonicus (Chloranthaceae) led to the isolation and identification of three new lindenane-type sesquiterpenoid dimers, chlorajaponilides F-H (1-3), along with seven known ones (4-10). Their chemical structures were established by extensive spectral evidence. Compounds 1 and 2 are both dimeric sesquiterpenoids featuring a rare hydroperoxy group at C-5. All compounds were tested for their activities on wild type HIV-1 replication and compounds 1, 2, 5, and 9 were effective with EC50 values from 3.08 to 17.16µM. All these four compounds showed the same inhibitory effects on the two NNRTI-resistant HIV strains as on wild-type HIV-1 with EC50 change folds from 0.61 to 1.6µM. Furthermore, compounds 1, 5, and 9 exhibited inhibitory activities on HCV replication with the similar potency as their activities on HIV-1. Our finding may provide a clue to address the problem of HIV-1 and HCV co-infection.
Assuntos
Antivirais/química , HIV-1/efeitos dos fármacos , Hepacivirus/efeitos dos fármacos , Magnoliopsida/química , Sesquiterpenos/química , Replicação Viral/efeitos dos fármacos , Antivirais/isolamento & purificação , Células HEK293 , HIV-1/fisiologia , Hepacivirus/fisiologia , Humanos , Estrutura Molecular , Sesquiterpenos/isolamento & purificaçãoRESUMO
Phytochemical investigation of the whole plants of Tacca plantaginea led to the isolation of 3 new withanolides and one new withanolide glucoside, named plantagiolides K-N (1-4), together with one known withanolide, 4 known withanolide glucosides, and 2 known taccalonolides. Their structures were elucidated by extensive spectroscopic analysis. Compound 4 is the first withanolide glycoside which the sugar moiety is attached at C-7. The effects of the some of isolates on TNFα-induced NF-κB transcriptional activity and cytotoxicity were evaluated.
Assuntos
Dioscoreaceae/química , Glucosídeos/química , Vitanolídeos/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Glucosídeos/isolamento & purificação , Células HEK293 , Células Hep G2 , Humanos , Concentração Inibidora 50 , Estrutura Molecular , NF-kappa B/metabolismo , Fator de Necrose Tumoral alfa/farmacologia , Vitanolídeos/isolamento & purificaçãoRESUMO
Two new cucurbitacins, endecaphyllacins A (1) and B (2), together with six known analogues (3-8), were isolated from the tubers of Hemsleya endecaphylla. The structures of 1 and 2 were elucidated by NMR and MS spectroscopic analysis. The relative stereochemistry of 1 was determined by single-crystal X-ray diffraction. Compound 4 (cucurbitacin B) showed potent anti-HIV-1 in C8166 cells (EC=0.09 microg/mL) with a selectivity index of 16.7.